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Gefitinib-based PROTAC 3
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Gefitinib-based PROTAC 3图片
CAS NO:2230821-27-7
包装与价格：
包装价格(元)
1mg电议
5mg电议
25mg电议

产品介绍
基于 Gefitinib 的 PROTAC 3 通过接头将 EGFR 结合元件与 von Hippel-Lindau 配体结合，在 HCC827（外显子 19 del）和 H3255（L858R 突变）细胞中诱导 EGFR 降解，DC50 分别为 11.7 nM 和 22.3 nM。
Cas No.2230821-27-7
分子式C47H57ClFN7O8S
分子量934.522
溶解度DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 16 mg/ml,Ethanol: 10 mg/ml
储存条件4°C, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1].

References:
[1]. Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.